Bi-Functional Co-Polymer Use for Ophthalmic and Other Topical and Local Applications

Abstract

The invention contemplates a copolymer which is a graft or block copolymer useful to change wettability and surface characteristics of biological surfaces. Methods for use of these formulations and coatings to change wettability and sterically stabilize, and lubricate biological surfaces in a subject, for example, in the treatment of dry eye syndrome, and to prevent adherence of unwanted proteins, for example in the treatment of contact lens intolerance, are provided.

We claim: 
     
         1 . A copolymer coated particle wherein the surface of said particle comprises a copolymer, said copolymer having (i) a binding moiety which is selected from the group consisting of positively charged, hydrophobic, and covalent; and (ii) a hydrophilic moiety. 
     
     
         2 . The copolymer coated particle of  claim 1 , wherein said copolymer coated particle further comprises an active agent. 
     
     
         3 . The copolymer coated particle of  claim 1 , wherein said copolymer coated particle further comprises an active agent for treating ophthalmic disease. 
     
     
         4 . The copolymer coated particle of  claim 3 , wherein said active agent is selected from the group consisting of an antibiotic, acetazolamide, antazoline, aspirin, atropine, azelastine, bacitracin, betaxolol, bimatoprost, a botanical drug, lutein, lycopene brimonodine, brinzolamide, carbachol, carteolol, ciprofloxacin, ofloxacin, cromalyn, cyclosporine, a cyclosporine pro-drug, a cyclosporine derivative, an immunomodulators, dapiprazole, dexamethasone, diclofenac, dipivifren, dorzolamide, epinephrine, erythromycin, fluoromethalone, flurbiprofen, gentamycin, a glaucoma medication, gramicidin, homatropine, hydrocortisone, hyoscine, keterolac, ibuprofen, ketotifen, latanaprost, levobunolol, levocabastine, levofloxin, lotepprednol, medrysone, methazolamide, metipranolol, naphazoline, natamycin, nedocromil, neomycin, neuroprotective agents, nonsteroidal anti-inflammatory agents, nepafanec, norfloxacin, ofloxacin olopatadine, oxymetazoline, pemirolast, pheniramine, phenylephrine, pilocarpine, povidone, prednisolone, proparacaine, scopolamine, tetracaine, steroids, sulfacetamide, tetrahydrozoline, hypertonic tears, timolal, tobramycin, travaprost, trifluridine, trimethiprim, tropicamide, unoprostone and zinc. 
     
     
         5 . The copolymer coated particle of  claim 4 , wherein said antibiotic is selected from the group consisting of fluoroquinolones, vancomycin, cephalosporin, gentamycin, erythromycin, azithromycin, sulfa drugs, bacitracin, gatifloxacin, levofloxin, moxifloxacin and ofloxacin. 
     
     
         6 . The copolymer coated particle of  claim 4 , wherein said glaucoma medication is selected from the group consisting of a prostaglandin, a carbonic anhydrase inhibitor, an epinephrine agonist, an alpha-agonist, and a beta-blocker. 
     
     
         7 . The copolymer coated particle of  claim 2 , wherein said active agent is selected from the group consisting of a drug and an allergen. 
     
     
         8 . The copolymer coated particle of  claim 7 , wherein said drug is selected from the group consisting of a small molecule, a chemical, a pharmaceutical and a biologic. 
     
     
         9 . The copolymer coated particle of  claim 7 , wherein said allergen is selected from the group consisting of a virus, a bacterium, a yeast and a prion. 
     
     
         10 . The copolymer coated particle of  claim 1 , wherein said copolymer coated particle has a diameter of less than or equal to 1 mm. 
     
     
         11 . The copolymer coated particle of  claim 10 , wherein said copolymer coated particle is designed for intramuscular injection. 
     
     
         12 . The copolymer coated particle of  claim 1 , wherein said copolymer coated particle has a diameter of less than or equal to 10 microns. 
     
     
         13 . The copolymer coated particle of  claim 12 , wherein said copolymer coated particle is designed for inhalation. 
     
     
         14 . The copolymer coated particle of  claim 1 , wherein said copolymer coated particle has a diameter of less than or equal to 1 micron. 
     
     
         15 . The copolymer coated particle of  claim 1 , wherein said particle is a drug or a drug particle. 
     
     
         16 . The copolymer coated particle of  claim 2 , wherein said active agent is contained within the particle, on the surface of the particle, in the copolymer coating of the particle, and/or on the surface of the copolymer coating of the particle. 
     
     
         17 . The copolymer coated particle of  claim 3 , wherein said active agent is contained within the particle, on the surface of the particle, in the copolymer coating of the particle, and/or on the surface of the copolymer coating of the particle. 
     
     
         18 . The copolymer coated particle of  claim 2 , wherein said active agent is selected from the group consisting of menthol and/or other numbing compound for treatment of coughs or sore throats.